The invention relates to the use of clindamycin palmitate for the production of pharmaceutical administration forms having a protracted release of the antibiotic active compound clindamycin and to corresponding administration forms, in particular in the form of shaped implants.
Clindamycin is an antibiotic of generally recognized value. It exhibits particular effectiveness against Gram-positive organisms such as staphylococci and streptococci and also against Gram-negative anaerobes. This antibiotic is therefore used for the treatment of a wide spectrum of diseases, e.g., in the control of infections of the digestive tract, the skin and the soft tissue and also in osteomyelitis and in gynecological infections. Clindamycin has furthermore been successfully employed in prophylaxis and therapy of bacterial endocarditis.
In the indications mentioned, this antibiotic is used in the form of physiologically acceptable salts such as, for example, clindamycin HCl, clindamycin phosphate ester or alternatively in the form of free clindamycin base.
Clindamycin is also known in the form of the palmitate ester. Clindamycin palmitate itself is microbiologically inactive. However, it is readily hydrolyzed by enzymes of the small intestine and the active clindamycin base is released from this form. The plasma half-life of the active compound is in this case about 2 hours. As a result of this property, clindamycin palmitate has found use in the form of the HCl salt, which is readily soluble in aqueous medium, as a rapid- and short-acting antibiotic in therapy forms where the active compound is administered orally. The free clindamycin palmitate ester (i.e., not in the form of the HCl salt) is virtually insoluble in aqueous media and therefore until now remained pharmacologically unimportant.